99 articles for thisTarget
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Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.

Array Biopharma
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.

Array Biopharma
Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2.

Array Biopharma
Discovery of 7-tetrahydropyran-2-yl chromans:ß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloidß-protein (Aß) in the central nervous system.

Array Biopharma
Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Array Biopharma
Identification of a new class of glucokinase activators through structure-based design.

Array Biopharma
Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species.

Array Biopharma
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Array Biopharma
Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors.

Array Biopharma
Discovery of spirocyclic sulfonamides as potent Akt inhibitors with exquisite selectivity against PKA.

Array Biopharma
Discovery of dihydrothieno- and dihydrofuropyrimidines as potent pan Akt inhibitors.

Array Biopharma
Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors.

Array Biopharma
Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.

Array Biopharma
Discovery and SAR of trisubstituted thiazolidinones as CCR4 antagonists.

Array Biopharma
Discovery and preclinical development of AR453588 as an anti-diabetic glucokinase activator.

Array Biopharma
Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.

Array Biopharma
Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity.

Array Biopharma
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.

Array Biopharma
Discovery of danoprevir (ITMN-191/R7227), a highly selective and potent inhibitor of hepatitis C virus (HCV) NS3/4A protease.

Array Biopharma
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 4: rational design and kinase selectivity profile of cell potent type II inhibitors.

Array Biopharma
Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.

Array Biopharma
The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.

Array Biopharma
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.

Array Biopharma
Pyrazolopyridine inhibitors of B-Raf(V600E). Part 3: an increase in aqueous solubility via the disruption of crystal packing.

Array Biopharma
Pyrazine derivative and application thereof in inhibiting SHP2

Suzhou Genhouse Pharmaceutical
CIS-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer

Amgen
Selective inhibitors of protein arginine methyltransferase 5 (PRMT5)

Prelude Therapeutics
Dipeptidyl ketoamide meta-methoxyphenyl derivatives and uses thereof

Landsteiner Genmed
Diazabicyclic substituted imidazopyrimidines and their use for the treatment of breathing disorders

Bayer Aktiengesellschaft
HDAC inhibitors for the treatment of diabetic peripheral neuropathy

Regenacy Pharmaceuticals
Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors

Xenon Pharmaceuticals
1-(3-aminopropyl) substituted cyclic amine compounds, preparation method therefor, and pharmaceutical compositions and uses thereof

Shanghai Institute of Material Medica, Chinese Academy of Sciences
Pyrrole six-membered heteroaryl ring derivative, preparation method thereof, and medicinal uses thereof

Jiangsu Hengrui Medicine
Cyclopentylbenzamide derivatives and their use for the treatment of psychotic and cognitive disorders

Takeda Pharmaceutical
Synthesis of a novel series of L-isoserine derivatives as aminopeptidase N inhibitors.

Shandong University
Synthesis and biological evaluation of novel N,N'-bis-methylenedioxybenzyl-alkylenediamines as bivalent anti-Alzheimer disease ligands.

Sun Yat-Sen University
Small-Molecule Inhibitors of the SOX18 Transcription Factor.

The University of Queensland
Pyrazole and imidazole derivatives useful as orexin antagonists

Actelion Pharmaceuticals
6-thio-substituted imidazo[1,2-a]pyrazines as Mps-1 inhibitors

Bayer Intellectual Property
Methods and compositions for studying, imaging, and treating pain

The Leland Stanford Junior University
Inhibitor Discovery for the Human GLUT1 from Homology Modeling and Virtual Screening.

Icahn School of Medicine At Mount Sinai
Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pryimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea

Vertex Pharmaceuticals
Repurposing human PDE4 inhibitors for neglected tropical diseases. Evaluation of analogs of the human PDE4 inhibitor GSK-256066 as inhibitors of PDEB1 of Trypanosoma brucei.

Northeastern University
4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics

Galderma Research & Development
Discovery of novel tricyclic pyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amine derivatives as VEGFR-2 inhibitors.

Suez Canal University
Solid-phase synthesis of a combinatorial array of 1,3-bis(acylamino)-2-butanones, inhibitors of the cysteine proteases cathepsins K and L.

Smithkline Beecham Pharmaceuticals
Inhibition of forskolin-induced neurite outgrowth and protein phosphorylation by a newly synthesized selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-(p-bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide (H-89), of PC12D pheochromocytoma cells.

Nagoya University School of Medicine
Synthesis and in vivo evaluation of a novel 5-HT1A receptor agonist radioligand [O-methyl- 11C]2-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl)-4-methyl-1,2,4-triazine-3,5(2H,4H)dione in nonhuman primates.

Columbia University
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid.

Istituto Di Chimica Biomolecolare
SAR of carbon-linked, 2-substituted purines: synthesis and characterization of AP23451 as a novel bone-targeted inhibitor of Src tyrosine kinase with in vivo anti-resorptive activity.

Ariad Pharmaceuticals
The discovery of novel vascular endothelial growth factor receptor tyrosine kinases inhibitors: pharmacophore modeling, virtual screening and docking studies.

Shanghai Jiao Tong University
A structure-guided approach to creating covalent FGFR inhibitors.

Harvard Medical School
Rational design, synthesis, and biological evaluation of progesterone-modified MRI contrast agents.

Northwestern University